Self-Assembly PEGylation Retaining Activity (SPRA) Technology via a Host-Guest Interaction Surpassing Conventional PEGylation Methods of Proteins.
作者： Tatsunori Hirotsu , Taishi Higashi , Irhan Ibrahim Abu Hashim , Shogo Misumi , Koki Wada
DOI: 10.1021/ACS.MOLPHARMACEUT.6B00678
关键词:
摘要: Polyethylene glycol (PEG) modification (PEGylation) is one of the best approaches to improve stabilities and blood half-lives protein drugs; however, PEGylation dramatically reduces bioactivities drugs. Here, we present “self-assembly retaining activity” (SPRA) technology via a host–guest interaction between PEGylated β-cyclodextrin (PEG-β-CyD) adamantane-appended (Ad) proteins. PEG-β-CyD formed stable complexes with Ad-insulin Ad-lysozyme yield SPRA-insulin SPRA-lysozyme, respectively. Both SPRA-proteins showed high stability against heat trypsin digest, comparable that covalently equivalents. Importantly, SPRA-lysozyme possessed ca. 100% lytic activity, whereas activity lysozyme was 23%. Additionally, provided prolonged peakless glucose profile when compared insulin glargine. It also no loss activity. In contrast, s...
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